申请人:Smallheer M. Joanne
公开号:US20050228000A1
公开(公告)日:2005-10-13
The present invention provides compounds of Formula (I):
or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, L
1
, L
2
, X
1
, X
2
, X
3
, X
4
, X
5
, R
4
, and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
本发明提供了化合物(I)的公式:或其立体异构体或药学上可接受的盐或溶剂形式,其中变量A、B、L1、L2、X1、X2、X3、X4、X5、R4和W的定义如本文所述。化合物(I)可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶酶的选择性抑制剂;例如凝血酶、因子Xa、因子XIa、因子IXa、因子VIIa和/或血浆激肽酶。特别是,它涉及选择性因子XIa抑制剂的化合物。本发明还涉及包含这些化合物的制药组合物以及使用它们治疗血栓栓塞和/或炎症性疾病的方法。